*Target (protein/gene name): serine threonine protein phosphatase 5 *Protein ID (NP or XP #): Tb927.10.13670 *Organism: trypanosoma brucei Etiologic Risk Group (see link below): Risk 2 *Background/Disease Information: Trypanosoma brucei is the protozoa that is the cause for the parasitic disease African trypanomiasis. This disease can infect both humans and animals, and is characterized by fever and headaches, until the lymphatic and circulatory systems become affected. The disease then progresses rapidly and has a variety of manifestations including severely disrupted sleep cycles due to the parasite passing through the blood brain barrier, anemia, endocrine malfunctions, cardiac problems and kidney dysfunctions. Druggable Target: A similar target has been used in successful runs by the study alsford, and the TDR gives it a druggability index of 0.5. It displays some similarity to a human, but not an exact match with 49% similarity on a 98% query coverage. http://www.tdrtargets.org/targets/view?gene_id=19618 Essentiality: *EC#: 3.1.3.16 Link to BRENDA EC# page: http://www.brenda-enzymes.org/php/result_flat.php4?ecno=3.1.3.16&Suchword=&organism[]=Trypanosoma+brucei&show_tm=0 Enzyme Assay information: http://www.sigmaaldrich.com/life-science/metabolomics/enzyme-explorer/learning-center/assay-library/ec-number-iii.html
Structure Available (PDB or Homology model)
Homology Model option:
---- Show pairwise alignment of your BLASTP search in NCBI against the PDB
---- Query Coverage: 98%
---- Max % Identities: 49%
---- % Positives: 68
Cartoon image of 1WAO, the closest protein resembling the chosen target. http://tritrypdb.org/tritrypdb/showRecord.do?name=GeneRecordClasses.GeneRecordClass&primary_key=Tb927.10.13670 http://www.rcsb.org/pdb/explore/explore.do?pdbId=1wao *Amino Acid Sequence:
MAGVEEADKLKQLGNAAFSERKWHLAIDMYTKAIELTKTPTLFCNRALAELRAELPGAAL
ADADAALGIEPTFAKAYYHKASAYLSLGKHKQALTNYKKVVDLAPQNSDAQAKVEFCKKE
IRRINFENAIMTPDEAPLSQTIKLGSVRADYDGPRIENETVTVEFVEAMKEHFRLEKLID
RHDVIFILLEVQKILKKCPNFVSINVPVGEEITVCGDTHGQYYDLLNIFKLNGNPLETNR
YLFNGDFVDRGSYSFENIMTLFAYKVLYPDHFFLSRGNHEGVSMNRMYGFEGEVTQKYNS
EMFRLFTEVFNSLPIGHIINNEVFVVHGGLYSSDKVTLDDLQHPNRFRDIPESGLICESL
WSDPQPMPGRAPSKRGVSCLSFGPDVTETFLNNNNLKLLVRSHEVKDEGYEIEHGGKCIT
VFSAPNYCDQMGNKGAFIRFTGGDMKPRFTTFTHVPHPGKRPMHYATGFGLF
*length of your protein in Amino Acids: 472 Molecular Weight of your protein in kiloDaltons using the Expasy ProtParamwebsite:
53312.7 Molar Extinction coefficient of your protein at 280 nm wavelength:
38320 TMpred graph Image (http://www.ch.embnet.org/software/TMPRED_form.html). *CDS Gene Sequence (paste as text only): *GC% Content for gene: *CDS Gene Sequence (codon optimized) - copy from output of Primer Design Protocol (paste as text only): *GC% Content for gene (codon optimized):
*Protein ID (NP or XP #): Tb927.10.13670
*Organism: trypanosoma brucei
Etiologic Risk Group (see link below): Risk 2
*Background/Disease Information:
Trypanosoma brucei is the protozoa that is the cause for the parasitic disease African trypanomiasis. This disease can infect both humans and animals, and is characterized by fever and headaches, until the lymphatic and circulatory systems become affected. The disease then progresses rapidly and has a variety of manifestations including severely disrupted sleep cycles due to the parasite passing through the blood brain barrier, anemia, endocrine malfunctions, cardiac problems and kidney dysfunctions.
Druggable Target: A similar target has been used in successful runs by the study alsford, and the TDR gives it a druggability index of 0.5. It displays some similarity to a human, but not an exact match with 49% similarity on a 98% query coverage.
http://www.tdrtargets.org/targets/view?gene_id=19618
Essentiality:
*EC#: 3.1.3.16
Link to BRENDA EC# page:
http://www.brenda-enzymes.org/php/result_flat.php4?ecno=3.1.3.16&Suchword=&organism[]=Trypanosoma+brucei&show_tm=0
Enzyme Assay information:
http://www.sigmaaldrich.com/life-science/metabolomics/enzyme-explorer/learning-center/assay-library/ec-number-iii.html
http://www.sigmaaldrich.com/content/dam/sigma-aldrich/docs/Sigma/Enzyme_Assay/calcineurin.pdf
Structure Available (PDB or Homology model)
Homology Model option:
---- Show pairwise alignment of your BLASTP search in NCBI against the PDB
---- Query Coverage: 98%
---- Max % Identities: 49%
---- % Positives: 68
Current Inhibitors: Only 5 hits were found in the binding database, the top hit being CHEMBL318778.
Expression Information: The protein is usually expressed via its natural protozoa, but has been cloned and characterized from e.coli before.
http://www.brenda-enzymes.org/literature/lit.php4?e=3.1.3.16&r=655670
Purification Method:
microcystin-Sepharose bead chromatography
http://www.brenda-enzymes.org/literature/lit.php4?e=3.1.3.16&r=694537
Image of protein:
Cartoon image of 1WAO, the closest protein resembling the chosen target.
http://tritrypdb.org/tritrypdb/showRecord.do?name=GeneRecordClasses.GeneRecordClass&primary_key=Tb927.10.13670
http://www.rcsb.org/pdb/explore/explore.do?pdbId=1wao
*Amino Acid Sequence:
MAGVEEADKLKQLGNAAFSERKWHLAIDMYTKAIELTKTPTLFCNRALAELRAELPGAAL
ADADAALGIEPTFAKAYYHKASAYLSLGKHKQALTNYKKVVDLAPQNSDAQAKVEFCKKE
IRRINFENAIMTPDEAPLSQTIKLGSVRADYDGPRIENETVTVEFVEAMKEHFRLEKLID
RHDVIFILLEVQKILKKCPNFVSINVPVGEEITVCGDTHGQYYDLLNIFKLNGNPLETNR
YLFNGDFVDRGSYSFENIMTLFAYKVLYPDHFFLSRGNHEGVSMNRMYGFEGEVTQKYNS
EMFRLFTEVFNSLPIGHIINNEVFVVHGGLYSSDKVTLDDLQHPNRFRDIPESGLICESL
WSDPQPMPGRAPSKRGVSCLSFGPDVTETFLNNNNLKLLVRSHEVKDEGYEIEHGGKCIT
VFSAPNYCDQMGNKGAFIRFTGGDMKPRFTTFTHVPHPGKRPMHYATGFGLF
*length of your protein in Amino Acids: 472
Molecular Weight of your protein in kiloDaltons using the Expasy ProtParamwebsite:
53312.7
Molar Extinction coefficient of your protein at 280 nm wavelength:
38320
TMpred graph Image (http://www.ch.embnet.org/software/TMPRED_form.html).
*CDS Gene Sequence (paste as text only):
*GC% Content for gene:
*CDS Gene Sequence (codon optimized) - copy from output of Primer Design Protocol (paste as text only):
*GC% Content for gene (codon optimized):